MK-0457, an Aurora kinase and BCR-ABL inhibitor, is active in patients with BCR-ABL T315I leukemia.

Abstract:

:MK-0457, an Aurora kinase and BCR-ABL inhibitor, was studied on a Phase I/II study in 77 patients with refractory hematologic malignancies. The average number of cycles per patient was 3 (range 1-21). Maximum tolerated doses for a 5-day short infusion and continuous infusion regimens were 40 mg/m(2)/h and 144 mg/m(2)/h, respectively. Drug-related adverse events (AEs) included transient mucositis and alopecia. Eight of 18 patients with BCR-ABL T315I-mutated chronic myelogenous leukemia (44%) had hematologic responses and one of three patients (33%) with Philadelphia chromosome-positive acute lymphoblastic leukemia obtained complete remission. MK-0457 has important activity in patients with leukemias expressing the highly resistant T315I BCR-ABL mutation.

journal_name

Leukemia

journal_title

Leukemia

authors

Giles FJ,Swords RT,Nagler A,Hochhaus A,Ottmann OG,Rizzieri DA,Talpaz M,Clark J,Watson P,Xiao A,Zhao B,Bergstrom D,Le Coutre PD,Freedman SJ,Cortes JE

doi

10.1038/leu.2012.186

subject

Has Abstract

pub_date

2013-01-01 00:00:00

pages

113-7

issue

1

eissn

0887-6924

issn

1476-5551

pii

leu2012186

journal_volume

27

pub_type

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